JP2016528242A5 - - Google Patents
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- Publication number
- JP2016528242A5 JP2016528242A5 JP2016533926A JP2016533926A JP2016528242A5 JP 2016528242 A5 JP2016528242 A5 JP 2016528242A5 JP 2016533926 A JP2016533926 A JP 2016533926A JP 2016533926 A JP2016533926 A JP 2016533926A JP 2016528242 A5 JP2016528242 A5 JP 2016528242A5
- Authority
- JP
- Japan
- Prior art keywords
- hemisulfate
- pharmaceutical composition
- represented
- purity
- methylene
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims description 16
- 238000005079 FT-Raman Methods 0.000 claims description 8
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 8
- QYNUQALWYRSVHF-OLZOCXBDSA-N (6R)-5,10-methylenetetrahydrofolic acid Chemical compound C([C@H]1CNC=2N=C(NC(=O)C=2N1C1)N)N1C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QYNUQALWYRSVHF-OLZOCXBDSA-N 0.000 claims description 6
- 239000013078 crystal Substances 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 238000002441 X-ray diffraction Methods 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 238000001228 spectrum Methods 0.000 claims description 4
- -1 lyophilizates Substances 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 239000007937 lozenge Substances 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims description 2
- 239000000829 suppository Substances 0.000 claims description 2
- 239000000725 suspension Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims 1
- 229960000304 folic acid Drugs 0.000 claims 1
- 235000019152 folic acid Nutrition 0.000 claims 1
- 239000011724 folic acid Substances 0.000 claims 1
- 239000002253 acid Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13004050.4A EP2837631A1 (en) | 2013-08-14 | 2013-08-14 | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| EP13004050.4 | 2013-08-14 | ||
| PCT/EP2014/067447 WO2015022407A1 (en) | 2013-08-14 | 2014-08-14 | Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018164332A Division JP6735321B2 (ja) | 2013-08-14 | 2018-09-03 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2019070293A Division JP6764501B2 (ja) | 2013-08-14 | 2019-04-02 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016528242A JP2016528242A (ja) | 2016-09-15 |
| JP2016528242A5 true JP2016528242A5 (https=) | 2017-12-14 |
| JP6617104B2 JP6617104B2 (ja) | 2019-12-04 |
Family
ID=48998397
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533926A Active JP6617104B2 (ja) | 2013-08-14 | 2014-08-14 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2018164332A Active JP6735321B2 (ja) | 2013-08-14 | 2018-09-03 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2019070293A Active JP6764501B2 (ja) | 2013-08-14 | 2019-04-02 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2020083208A Active JP7396960B2 (ja) | 2013-08-14 | 2020-05-11 | ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2021183793A Active JP7710356B2 (ja) | 2013-08-14 | 2021-11-11 | ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸のヘミ硫酸塩 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018164332A Active JP6735321B2 (ja) | 2013-08-14 | 2018-09-03 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2019070293A Active JP6764501B2 (ja) | 2013-08-14 | 2019-04-02 | ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2020083208A Active JP7396960B2 (ja) | 2013-08-14 | 2020-05-11 | ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸のヘミ硫酸塩 |
| JP2021183793A Active JP7710356B2 (ja) | 2013-08-14 | 2021-11-11 | ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸のヘミ硫酸塩 |
Country Status (27)
| Country | Link |
|---|---|
| US (4) | US20160185787A1 (https=) |
| EP (3) | EP2837631A1 (https=) |
| JP (5) | JP6617104B2 (https=) |
| KR (2) | KR102410373B1 (https=) |
| CN (2) | CN108096200A (https=) |
| AU (2) | AU2014307872B2 (https=) |
| BR (2) | BR122020002802B1 (https=) |
| CA (1) | CA2921178C (https=) |
| CY (2) | CY1119694T1 (https=) |
| DK (2) | DK3033344T3 (https=) |
| EA (3) | EA202091271A3 (https=) |
| ES (2) | ES2871483T3 (https=) |
| HK (1) | HK1256262A1 (https=) |
| HR (2) | HRP20171895T1 (https=) |
| HU (2) | HUE037615T2 (https=) |
| IL (2) | IL244069B (https=) |
| LT (2) | LT3287460T (https=) |
| MX (2) | MX382578B (https=) |
| NO (1) | NO3033344T3 (https=) |
| NZ (2) | NZ745811A (https=) |
| PL (2) | PL3287460T3 (https=) |
| PT (2) | PT3287460T (https=) |
| RS (2) | RS61986B1 (https=) |
| SG (2) | SG11201601016PA (https=) |
| SI (2) | SI3033344T1 (https=) |
| WO (1) | WO2015022407A1 (https=) |
| ZA (1) | ZA201509204B (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| US10059710B2 (en) | 2016-02-17 | 2018-08-28 | Merck & Cie | Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid |
| EP3446704A1 (en) * | 2017-08-24 | 2019-02-27 | Isofol Medical AB | [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy |
| EP3446703A1 (en) * | 2017-08-24 | 2019-02-27 | Isofol Medical AB | 6r]-mthf multiple bolus administration in 5-fluorouracil based chemotherapy |
| DK3668516T3 (da) | 2017-08-16 | 2021-12-13 | Merck Patent Gmbh | Stabile lyofilisater omfattende 5,10-methylen-(6r)-tetrahydrofolsyre og en dicarboxylsyre |
| JP7258759B2 (ja) * | 2018-01-05 | 2023-04-17 | アイソフォル・メディカル・エービー | 大腸癌及び転移性大腸癌を治療する方法 |
| CN115335740A (zh) * | 2020-03-30 | 2022-11-11 | 住友化学株式会社 | 层叠体 |
| CN119343131A (zh) | 2022-06-08 | 2025-01-21 | 默克专利股份有限公司 | 包含5,10-亚甲基-(6r)-四氢叶酸钠的浓缩溶液 |
| CN119325374A (zh) | 2022-06-08 | 2025-01-17 | 默克专利股份有限公司 | 包含5,10-亚甲基-(6r)-四氢叶酸的稳定的冻干物 |
| US20250360135A1 (en) | 2022-06-08 | 2025-11-27 | Merck Patent Gmbh | Compositions comprising disodium 5,10-methylene-(6r)-tetrahydrofolate |
| EP4536185A1 (en) | 2022-06-08 | 2025-04-16 | Merck Patent GmbH | Stable pharmaceutical compositions comprising 5,10-methylene-(6r)-tetrahydrofolic acid and nacl |
| US20260000671A1 (en) | 2022-06-08 | 2026-01-01 | Merck Patent Gmbh | Concentrated solutions comprising 5,10-methylene-(6r)-tetrahydrofolic acid |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2300505A (en) * | 1940-10-31 | 1942-11-03 | Bell Telephone Labor Inc | Selective system |
| CA1215945A (en) | 1983-03-20 | 1986-12-30 | Bengt Gustavsson | Fluid transfer system |
| DE3821875C1 (https=) * | 1988-06-29 | 1990-02-15 | Eprova Ag, Forschungsinstitut, Schaffhausen, Ch | |
| CH682664A5 (en) * | 1991-10-15 | 1993-10-29 | Eprova Ag | Stable salts of 5,10-methylene tetrahydrofolate. |
| CH684644A5 (de) | 1992-07-13 | 1994-11-15 | Eprova Ag | 5,10-Methylentetrahydrofolsäure-Cyclodextrin-Einschlussverbindungen. |
| HU226998B1 (en) | 2000-11-23 | 2010-04-28 | Richter Gedeon Nyrt | Desloratadine hemisulphate, process for the preparation thereof and pharmaceutical compositions containing the same |
| CH696628A5 (de) * | 2002-02-26 | 2007-08-31 | Eprova Ag | Verwendung von Folaten zur Herstellung einer Zubereitung geeignet zur Vorbeugung und Behandlung von Entzündungen und entzündungsassoziierter Krankheiten, im Speziellen zur Beeinflussung der |
| CH697021A5 (de) | 2003-06-26 | 2008-03-31 | Merck Eprova Ag | Stabile pharmazeutische Zusammensetzungen von 5, 10-Methylentetrahydrofolat. |
| EP1968551A2 (en) | 2005-12-02 | 2008-09-17 | Adventrx Pharmaceuticals, Inc. | Stable pharmaceutical compositions of 5,10 methylenetetrahydrofolate |
| ES2577391T3 (es) | 2006-12-21 | 2016-07-14 | F. Hoffmann-La Roche Ag | Polimorfos de un antagonista del receptor mglur5 |
| JP5294968B2 (ja) | 2009-05-01 | 2013-09-18 | 三星ダイヤモンド工業株式会社 | スクライブヘッド及び該スクライブヘッドを用いたスクライブ装置 |
| CN110200963A (zh) * | 2011-10-19 | 2019-09-06 | 墨卡托医疗系统公司 | 局部调节组织和细胞以提高疗效包括肾去神经支配 |
| EP2837766A1 (de) * | 2013-08-14 | 2015-02-18 | Sika Technology AG | Verfahren zum Ausfüllen einer Fuge mit einem Kleb- und/oder Dichtstoff sowie System zum Ausfüllen einer Fuge mit einem Kleb- und/oder Dichtstoff |
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| JP6971761B2 (ja) * | 2017-10-11 | 2021-11-24 | 株式会社Ｉｈｉプラント | タンクの構築方法 |
-
2013
- 2013-08-14 EP EP13004050.4A patent/EP2837631A1/en not_active Withdrawn
-
2014
- 2014-08-14 SG SG11201601016PA patent/SG11201601016PA/en unknown
- 2014-08-14 HU HUE14758102A patent/HUE037615T2/hu unknown
- 2014-08-14 NO NO14758102A patent/NO3033344T3/no unknown
- 2014-08-14 SG SG10201801179VA patent/SG10201801179VA/en unknown
- 2014-08-14 PT PT171902794T patent/PT3287460T/pt unknown
- 2014-08-14 BR BR122020002802-5A patent/BR122020002802B1/pt active IP Right Grant
- 2014-08-14 LT LTEP17190279.4T patent/LT3287460T/lt unknown
- 2014-08-14 EA EA202091271A patent/EA202091271A3/ru unknown
- 2014-08-14 HR HRP20171895TT patent/HRP20171895T1/hr unknown
- 2014-08-14 BR BR112016002770-1A patent/BR112016002770B1/pt active IP Right Grant
- 2014-08-14 MX MX2018013134A patent/MX382578B/es unknown
- 2014-08-14 SI SI201430529T patent/SI3033344T1/en unknown
- 2014-08-14 NZ NZ745811A patent/NZ745811A/en unknown
- 2014-08-14 CN CN201810160334.3A patent/CN108096200A/zh active Pending
- 2014-08-14 CA CA2921178A patent/CA2921178C/en active Active
- 2014-08-14 KR KR1020217009189A patent/KR102410373B1/ko active Active
- 2014-08-14 WO PCT/EP2014/067447 patent/WO2015022407A1/en not_active Ceased
- 2014-08-14 SI SI201431825T patent/SI3287460T1/sl unknown
- 2014-08-14 MX MX2016001834A patent/MX360355B/es active IP Right Grant
- 2014-08-14 HU HUE17190279A patent/HUE054504T2/hu unknown
- 2014-08-14 EA EA201600172A patent/EA032179B1/ru not_active IP Right Cessation
- 2014-08-14 RS RS20210630A patent/RS61986B1/sr unknown
- 2014-08-14 JP JP2016533926A patent/JP6617104B2/ja active Active
- 2014-08-14 PT PT147581029T patent/PT3033344T/pt unknown
- 2014-08-14 CN CN201480044477.8A patent/CN105452250B/zh active Active
- 2014-08-14 PL PL17190279T patent/PL3287460T3/pl unknown
- 2014-08-14 NZ NZ71782514A patent/NZ717825A/en unknown
- 2014-08-14 PL PL14758102T patent/PL3033344T3/pl unknown
- 2014-08-14 US US14/912,328 patent/US20160185787A1/en not_active Abandoned
- 2014-08-14 KR KR1020167006595A patent/KR102439605B1/ko active Active
- 2014-08-14 RS RS20171337A patent/RS56910B1/sr unknown
- 2014-08-14 EA EA201892729A patent/EA201892729A1/ru unknown
- 2014-08-14 ES ES17190279T patent/ES2871483T3/es active Active
- 2014-08-14 EP EP14758102.9A patent/EP3033344B1/en active Active
- 2014-08-14 ES ES14758102.9T patent/ES2654474T3/es active Active
- 2014-08-14 AU AU2014307872A patent/AU2014307872B2/en active Active
- 2014-08-14 EP EP17190279.4A patent/EP3287460B1/en active Active
- 2014-08-14 DK DK14758102.9T patent/DK3033344T3/en active
- 2014-08-14 DK DK17190279.4T patent/DK3287460T3/da active
- 2014-08-14 LT LTEP14758102.9T patent/LT3033344T/lt unknown
-
2015
- 2015-12-17 ZA ZA2015/09204A patent/ZA201509204B/en unknown
-
2016
- 2016-02-11 IL IL244069A patent/IL244069B/en active IP Right Grant
-
2017
- 2017-12-12 CY CY20171101298T patent/CY1119694T1/el unknown
-
2018
- 2018-09-03 JP JP2018164332A patent/JP6735321B2/ja active Active
- 2018-11-29 HK HK18115320.9A patent/HK1256262A1/zh unknown
- 2018-12-06 US US16/212,056 patent/US20190106431A1/en not_active Abandoned
- 2018-12-13 AU AU2018278943A patent/AU2018278943B2/en active Active
-
2019
- 2019-04-02 JP JP2019070293A patent/JP6764501B2/ja active Active
- 2019-09-08 IL IL269170A patent/IL269170B/en active IP Right Grant
-
2020
- 2020-05-11 JP JP2020083208A patent/JP7396960B2/ja active Active
-
2021
- 2021-04-27 CY CY20211100364T patent/CY1124076T1/el unknown
- 2021-05-12 HR HRP20210743TT patent/HRP20210743T1/hr unknown
- 2021-10-08 US US17/496,939 patent/US12122783B2/en active Active
- 2021-11-11 JP JP2021183793A patent/JP7710356B2/ja active Active
-
2024
- 2024-08-09 US US18/799,606 patent/US20240400574A1/en active Pending
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